专利快速检索-快速检索全球专利，免费商用专利数据库-IPRDB

31. 发明授权

US4397848A N-Substituted aziridine-2-carboxylic acid immunostimulant derivatives 失效
标题翻译： N-取代的氮丙啶-2-羧酸免疫刺激剂衍生物
公开(公告)号：US4397848A
公开(公告)日：1983-08-09
申请号：US236375
申请日：1981-02-20
申请人： Elmar Bosies , Wolfgang Kampe , Max Thiel , Uwe Bicker , Dietmar Boerner
发明人： Elmar Bosies , Wolfgang Kampe , Max Thiel , Uwe Bicker , Dietmar Boerner
IPC分类号： A61K31/395 , A61K31/396 , A61K31/44 , A61K31/4427 , A61K31/443 , A61K31/505 , A61P35/00 , A61P37/00 , A61P37/06 , C07D203/22 , C07D401/12 , C07D403/12 , C07D405/12
CPC分类号： C07D203/22 , Y10S514/885
摘要： The present invention provides pharmaceutical compositions containing N-substituted aziridine-2-carboxylic acid derivatives of the general formula: ##STR1## wherein X is a carboxyl, a cyano, an alkoxycarbonyl or an optionally substituted carbamoyl radical, R is a hydrogen atom, or an optionally substituted aliphatic hydrocarbon radical or cycloalkyl or cycloalkenyl radical, and R.sub.1 is a hydrogen atom or an alkyl or phenyl radical; and the pharmacologically acceptable salts thereof, in admixture with a pharmaceutical diluent or carrier. The present invention also provides, as new compounds, N-substituted aziridine-2-carboxylic acid derivatives of general formula (I') but with the proviso that when X is a carbamoyl or alkoxycarbonyl radical and R.sub.1 is a hydrogen atom, R is not a methyl, ethyl, isopropyl or benzyl radical; and the pharmacologically acceptable salts thereof, and also provides processes for the preparation of these new compounds. Furthermore, the present invention is concerned with the use of the compounds of general formula (I') and of the pharmacologically acceptable salts thereof for combating diseases associated with a weakening of the immune system.
摘要翻译：本发明提供含有下列通式的N-取代的氮丙啶-2-羧酸衍生物的药物组合物：其中X是羧基，氰基，烷氧基羰基或任选取代的氨基甲酰基，R是氢原子或任选取代的脂族烃基或环烷基或环烯基，R 1为氢原子或烷基或苯基; 和其药学上可接受的盐，与药物稀释剂或载体混合。本发明还提供了作为新化合物的通式（I'）的N-取代的氮丙啶-2-羧酸衍生物，但条件是当X是氨基甲酰基或烷氧基羰基并且R 1是氢原子时，R不是甲基，乙基，异丙基或苄基; 及其药理学上可接受的盐，也提供制备这些新化合物的方法。此外，本发明涉及通式（I'）的化合物及其药理学上可接受的盐在与免疫系统的弱化相关的疾病中的用途。

32. 发明授权

US4370323A 2-Cyanoaziridinyl-(1)-2-substituted-aziridinyl-(1)-methanes 失效
标题翻译： 2-氰基氮丙啶基 - （1）-2-取代的吖丙啶基 - （1） - 甲烷
公开(公告)号：US4370323A
公开(公告)日：1983-01-25
申请号：US776068
申请日：1977-03-09
申请人： Wolfgang Kampe , Max Thiel , Erich Fauland , Uwe Bicker , Gottfried Hebold
发明人： Wolfgang Kampe , Max Thiel , Erich Fauland , Uwe Bicker , Gottfried Hebold
IPC分类号： C07D203/06 , A61K31/395 , A61K31/396 , A61K31/435 , A61P35/00 , A61P37/04 , C07D203/08 , C07D203/12 , C07D203/14 , C07D333/00 , C07D335/00 , C07D403/14 , C07D405/14 , C07D409/14 , C07D451/14 , C07D403/06 , C07D401/14
CPC分类号： C07D203/08 , C07D451/14 , Y10S514/885
摘要： A 2-cyanoaziridinyl-(1)-2-substituted-aziridinyl-(1)-methane ##STR1## wherein R is a nitrile or carbamoyl group, andR.sub.1 and R.sub.2 each independently is a hydrogen atom, an aliphatic hydrocarbon radical containing up to 10 carbon atoms optionally substituted by hydroxyl, alkoxy, amino, alkylamino, dialkylamino, alkoxycarbonyl, cyano, 1, 2 or 3 halogens, cycloalkyl, phenyl or phenoxy; nitrile, carboxyl, alkoxycarbonyl or optionally hydrogenated monocyclic heteroaryl or phenyl optionally substituted by alkyl, alkoxy, hydroxy, alkoxcarbonyl, dialkylamino, alkylthio, trifluoromethyl, nitro, carbamoyl, nitrile, sulphonamido, hydroxyalkyl, methylenedioxy, or halogen; or R.sub.1 and R.sub.2, together with the carbon atom to which they are attached, form a ring containing up to 8 ring members of which at least one may be oxygen, sulphur, SO, SO.sub.2 NH, N-alkyl, N-acyl or N-alkoxycarbonylalkyl, and which can be substituted by alkyl, alkoxy, hydroxyl, alkylenedioxy, alkoxycarbonyl, hydroxyalkyl, alkoxycarbonylalkyl, dialkylamino, oxo or 2-cyanoaziridino groups, or can be fused to 1 or 2 benzene rings or can be bridged by alkylene radicals containing up to 3 carbon atoms.The compounds are characterized by cytostatic and immune response-stimulating activity.
摘要翻译： 2-氰基氮丙啶基 - （1）-2-取代的吖丙啶基 - （1） - 甲烷，其中R是腈或氨基甲酰基，R 1和R 2各自独立地为氢原子，含有至多任选被羟基，烷氧基，氨基，烷基氨基，二烷基氨基，烷氧基羰基，氰基，1,2或3卤素，环烷基，苯基或苯氧基取代的10个碳原子; 腈，羧基，烷氧基羰基或任选氢化的单环杂芳基或任选被烷基，烷氧基，羟基，烷氧基羰基，二烷基氨基，烷硫基，三氟甲基，硝基，氨基甲酰基，腈，磺酰胺基，羟烷基，亚甲二氧基或卤素取代的苯基。或R 1和R 2与它们所连接的碳原子一起形成含有至多8个环成员的环，其中至少一个可以是氧，硫，SO，SO 2 + L，NH，N-烷基，酰基或N-烷氧基羰基烷基，其可以被烷基，烷氧基，羟基，亚烷基二氧基，烷氧基羰基，羟基烷基，烷氧基羰基烷基，二烷基氨基，氧代或2-氰基氮丙啶基取代，或者可以与1或2个苯环稠合，或可以被含有至多3个碳原子的亚烷基。该化合物的特征在于细胞抑制和免疫应答刺激活性。

33. 发明授权

US4143149A Indazolyl-(4)-oxypropanolamine compounds and therapeutic compositions 失效
标题翻译：（4） - 异丙醇胺化合物和治疗组合物
公开(公告)号：US4143149A
公开(公告)日：1979-03-06
申请号：US790648
申请日：1977-04-25
申请人： Fritz Wiedemann , Wolfgang Kampe , Max Thiel , Wolfgang Bartsch , Egon Roesch
发明人： Fritz Wiedemann , Wolfgang Kampe , Max Thiel , Wolfgang Bartsch , Egon Roesch
IPC分类号： A61K31/415 , A61P9/00 , A61P25/02 , C07D231/56
CPC分类号： C07D231/56
摘要： New indazolyl-(4)-oxypropanolamine compounds of the formula ##STR1## wherein R.sub.1 is hydrogen or lower alkyl; andR.sub.2 is straight-chain or branched lower alkyl which can be substituted by lower alkylthio;And the pharmacologically compatible salts thereof; are outstandingly effective adrenergic .beta.-receptor inhibitors and useful in the treatment or prevention of a recurrence of cardiac and circulatory diseases.

34. 发明授权

US4029783A N-substituted 1-amino-3-phenoxy-propan-2-ol compounds and therapeutic compositions containing them 失效
标题翻译： N-取代的1-氨基-3-苯氧基 - 丙-2-醇化合物和含有它们的治疗组合物
公开(公告)号：US4029783A
公开(公告)日：1977-06-14
申请号：US638874
申请日：1975-12-08
申请人： Fritz Wiedemann , Max Thiel , Kurt Stach , Karl Dietmann , Gisbert Sponer
发明人： Fritz Wiedemann , Max Thiel , Kurt Stach , Karl Dietmann , Gisbert Sponer
IPC分类号： C07D209/86 , A61K31/54 , C07D279/24
CPC分类号： C07D209/86
摘要： New N-substituted 1-amino-3-phenoxy-propan-2-ol compounds of the formula: ##STR1## wherein R.sub.1 and R.sub.2 are, individually, hydrogen or, taken together, represent a sulfur linkage, an ethylene radical or a valency bond;B is straight or branched chain alkylene or hydroxyalkylene of from 2 to 5 carbon atoms; andR.sub.3 is hydrogen or alkyl of up to 3 carbon atoms;And the physiologically compatible salts thereof; possess valuable cardiac and circulatory activity.
摘要翻译：新的N-取代的1-氨基-3-苯氧基 - 丙-2-醇，其分子式为：其中R 1和R 2各自为氢或一起表示硫键，乙烯激进或价格债券; B是2至5个碳原子的直链或支链亚烷基或羟基亚烷基; 并且R 3是氢或至多3个碳原子的烷基; 及其生理适应性肥皂; 有价值的心脏和循环活动。

35. 发明授权

US3968129A Azidophenol amine compounds and therapeutic compositions 失效
标题翻译：叠氮酚胺化合物和治疗组合物
公开(公告)号：US3968129A
公开(公告)日：1976-07-06
申请号：US544720
申请日：1975-01-28
申请人： Wolfgang Kampe , Kurt Stach , Max Thiel , Wolfgang Bartsch , Karl Dietmann
发明人： Wolfgang Kampe , Kurt Stach , Max Thiel , Wolfgang Bartsch , Karl Dietmann
IPC分类号： C07C247/16 , A61K20060101 , A61K31/13 , A61K31/135 , A61K31/655 , A61P9/00 , C07C20060101 , C07C67/00 , C07C217/32 , C07C241/00 , C07D303/22 , C07C117/00
CPC分类号： C07C247/00
摘要： New amine derivatives of azidophenols having the formula: ##EQU1## wherein R is straight-chained or branched alkyl;And the pharmacologically compatible salts thereof;Inhibit adrenogenic .beta.-receptors and are suitable for the treatment and prophylaxis of cardiac and circulatory diseases.
摘要翻译：具有下式的叠氮酚的新胺衍生物：OH | O-CH 2 -CH-CH 2 -NH-R（I）其中R是直链或支链烷基; 及其药理学兼容性; 抑制ADRENOGENICβ受体，适用于治疗和预防心脏病和循环性疾病。

36. 发明授权

US3962242A 3-(5-Nitro-2-furyl)-6-cyano-s-triazolo(4,3-b)pyridazine 失效
标题翻译： 3-（5-硝基-2-呋喃基）-6-氰基-S-三唑（4,3-B）吡啶
公开(公告)号：US3962242A
公开(公告)日：1976-06-08
申请号：US545661
申请日：1975-01-30
申请人： Herbert Berger , Rudi Gall , Max Thiel , Wolfgang Vomel , Winfriede Sauer
发明人： Herbert Berger , Rudi Gall , Max Thiel , Wolfgang Vomel , Winfriede Sauer
IPC分类号： C07D487/04 , C07D237/26
CPC分类号： C07D487/04
摘要： Nitrofuryl-triazolo[4,3-b]pyridazine compounds of the formula ##SPC1##WhereinR.sub.1 is lower alkoxy radical or a saturated 5- or 6-membered heterocyclic ring attached via a cyclic nitrogen atom, which heterocyclic ring can also contain, in addition to said cyclic nitrogen atom, a cyclic oxygen atom or an optionally lower alkylated cyclic nitrogen atom and R.sub.2 is a hydrogen atom or R.sub.1 and R.sub.2 together represent an additional valency bond,Are outstandingly effective as bacteriostats and are particularly useful in the treatment of bacterial infections in the urinary tract.

你已经成功收藏专利！

检索式保存成功!

IPRDB

热门服务

关于我们

友情链接

联系方式